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编 号:F540756
分子式:C31H40N4O7
分子量:580.67
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1.

体内研究:
ONX-0914 (2-10 mg/kg;静脉注射;在第 4、6 和 8 天) 改善小鼠关节炎的疾病。 ONX-0914 (第 2、6 和在第 25、27、29、31 和 33 天,每公斤体重 10 毫克;iv) 处理还在 T 和 B 细胞依赖性 CIA (胶原诱导的关节炎) 模型中诱导了快速处理反应。Animal Model:Collagen antibody-induced arthritis (CAIA, Arthritis was induced in BALB/c mice with antibodies specific for type II collagen (mAb) and endotoxin)
Dosage:2, 6 or 10 mg per kg body weight
Administration:I.v.; treated on days 4, 6 and 8
Result:Blocked disease progression in a dose-dependent manner and completely ameliorated visible signs of disease at the highest dose.

体外研究:
ONX-0914 抑制 LMP7 特异性抗原呈递。ONX-0914 阻断小鼠脾细胞产生细胞因子并阻断 T 细胞分化。
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